1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. Osimertinib dimesylate

Osimertinib dimesylate (Synonyms: AZD-9291 (dimesylate); Mereletinib (dimesylate))

Cat. No.: HY-79077 Purity: 99.96%
Handling Instructions

Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.

For research use only. We do not sell to patients.

Osimertinib dimesylate Chemical Structure

Osimertinib dimesylate Chemical Structure

CAS No. : 2070014-82-1

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Customer Review

Based on 38 publication(s) in Google Scholar

Other Forms of Osimertinib dimesylate:

Top Publications Citing Use of Products

    Osimertinib dimesylate purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. 

    Measurement of antiproliferation effects of AZD9291 by EdU incorporation assay.

    Osimertinib dimesylate purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. 

    U87 and U251 cells are exposed to indicated concentrations of AZD9291 for 24 h and then stimulated with EGF (100 ng/mL) for 30 min. Cell lysates are prepared and examined using Western blot analysis with indicated antibodies.

    Osimertinib dimesylate purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219. 

    U87 and U251 cells are treated with AZD9291 or CP-358774 for 4, 24 and 48 h. The expression level of p-ERK are assessed using Western blot analysis.

    Osimertinib dimesylate purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22.

    Effect of PCI-32765, WZ4002, AZD9291 and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.

    Osimertinib dimesylate purchased from MCE. Usage Cited in: Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4.

    Negligible increases in caspase-3 activity or PARP-1 cleavage is observed in H1975 NSCLC cells treated with DMSO, single agent PAC-1 (5 mM), or Osimertinib (Osi). In cells treated with PAC-1+Osimertinib, dramatic increases in caspase-3 activity is observed as early as 36 hr post treatment.

    Osimertinib dimesylate purchased from MCE. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372.

    In all of the cell lines tested, AZD9291 significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

    Osimertinib dimesylate purchased from MCE. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372.

    In all of the cell lines tested, AZD9291 significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

    Osimertinib dimesylate purchased from MCE. Usage Cited in: Environ Toxicol. 2019 Jan 8. 

    Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib dimesylate purchased from MCE. Usage Cited in: Environ Toxicol. 2019 Jan 8. 

    Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib dimesylate purchased from MCE. Usage Cited in: Environ Toxicol. 2019 Jan 8. 

    Protein levels of NF-κB and IκB are analyzed are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib dimesylate purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 Jun 6. 

    MDAMB-453 cells are pre-treated with 10 μM MG132 for 1 h before treatment with the 20 μM AZD for 4 h. Cell lysates were used for SDS PAGE and Western blotting. AZD9291 disrupts the EZH2–EED interaction by binding to EZH2 directly
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    Description

    Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively.

    IC50 & Target[1]

    EGFRL858R

    12 nM (IC50)

    EGFRL858R/T790M

    1 nM (IC50)

    In Vitro

    Osimertinib (AZD-9291) shows similar potency to early generation tyrosine kinase inhibitor (TKIs) in inhibiting EGFR phosphorylation in EGFR cells harboring sensitising EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del), with mean IC50 values ranging from 13 to 54 nM for Osimertinib (AZD-9291). Osimertinib (AZD-9291) also potently inhibits phosphorylation of EGFR in T790M mutant cell lines (H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC50 potency less than 15 nM[1].

    In Vivo

    The tumor-bearing mice are treated with Osimertinib (AZD-9291) (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice displays nearly 80% reduction in tumor volume by magnetic resonance imaging MRI after therapy with Osimertinib (AZD-9291), while 5 of 5 mice treated with vehicle shows tumor growth[1]. Osimertinib (AZD-9291) demonstrates improved rat PK, reduced hERG affinity, and improved IGF1R margins relative to the previously described compounds, and so this compound is selected for further investigation. Osimertinib (AZD-9291) also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing Osimertinib (AZD-9291) in three efficacy models, The comparable efficacy is observed at relatively low doses (10 mg/kg per day). The excellent efficacy is also observed when Osimertinib (AZD-9291) is dosed at 5 mg/kg per day[2].

    Clinical Trial
    Molecular Weight

    691.82

    Formula

    C₃₀H₄₁N₇O₈S₂

    CAS No.

    2070014-82-1

    SMILES

    CS(=O)(O)=O.C=CC(NC1=CC(NC2=NC=CC(C3=CN(C)C4=C3C=CC=C4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O.CS(=O)(O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 0.4 mg/mL (0.58 mM; Need ultrasonic and warming)

    References
    Cell Assay
    [1]

    PC-9 cells are seeded into T75 flasks (5×105 cells/flask) in RPMI growth media and incubated at 37°C, 5% CO2. The following day the media is replaced with media supplemented with a concentration of EGFR inhibitor equal to the EC50 concentration predetermined in PC-9 cells. Media changes are carried out every 2-3 days and resistant clones allowed to grow to 80% confluency prior to the cells being trypsinised and reseeded at the original seeding density in media containing twice the concentration of EGFR inhibitor. Dose escalations are continued until a final concentration of 1.5 μM ZD1839, 1.5 μM BIBW 2992, 1.5 μM WZ4002 or 160 nM Osimertinib (AZD-9291) are achieved[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1][2]

    Mice[1]
    The EGFRL858R and EGFRL858R+T790M mice (male and female) are used. Osimertinib (AZD-9291) is suspended in 1% Polysorbate 80 and administered via oral gavage once daily at the doses of 7.5 mg/kg and 5 mg/kg, respectively. Mice are imaged weekly at the Vanderbilt University Institute of Imaging Science. For immunoblot analysis, mice are treated for eight hours with drug as described before dissection and flash freezing of the lungs. Lungs are pulverized in liquid nitrogen before lysis.
    Rats[2]
    The male RccHan:WIST rats (10-week-old) are received a single oral dose of Osimertinib (AZD-9291) (200 mg/kg). Blood glucose levels are measured using an Accuchek Active meter.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
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    Keywords:

    Osimertinib dimesylateAZD-9291 dimesylateMereletinib dimesylateEGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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